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13 条记录 (耗时 0.025 秒)

    1,3-dioxane derivatives having protein kinase C inhibitory activity
    1.
    发明授权
    1,3-dioxane derivatives having protein kinase C inhibitory activity 失效
    具有蛋白激酶C抑制活性的1,3-二恶烷衍生物

    公开(公告)号：US5360818A

    公开(公告)日：1994-11-01

    申请号：US110847

    申请日：1993-08-24

    申请人： Jack B. Jiang ,  Mary G. Johnson ,  Jeffrey Nichols

    发明人： Jack B. Jiang ,  Mary G. Johnson ,  Jeffrey Nichols

    IPC分类号： C07D319/06 ,  A61K31/35 ,  C07D309/14

    CPC分类号： C07D319/06

    摘要： The present invention provides compounds having the formula ##STR1## wherein R.sub.1 is alkyl, alkenyl and alkynyl having from 2 to about 20 carbon atoms; R.sub.2, R.sub.3 and R.sub.6 are independently H, phenyl or alkyl having from 1 to about 20 carbon atoms; and R.sub.4 and R.sub.5 are independently H, R.sub.6 imino, or amidino, and pharmaceutically acceptable salts thereof which are useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

    摘要翻译： 本发明提供了具有式“IMAGE”的化合物，其中R 1是具有2至约20个碳原子的烷基，烯基和炔基; R2，R3和R6独立地为H，苯基或具有1至约20个碳原子的烷基; 和R4和R5独立地是H，R6亚氨基或脒基，及其药学上可接受的盐，其可用于抑制蛋白激酶C，并且治疗与抑制蛋白激酶C特别是癌症肿瘤，炎性疾病，再灌注损伤有关或受其影响的病症 ，以及与再灌注损伤相关的心脏功能障碍。

    Furo-coumarinsulfonamides as protein kinase C inhibitors
    2.
    发明授权
    Furo-coumarinsulfonamides as protein kinase C inhibitors 失效
    呋喃香豆素磺酰胺作为蛋白激酶C抑制剂

    公开(公告)号：US5216014A

    公开(公告)日：1993-06-01

    申请号：US757664

    申请日：1991-09-10

    申请人： Jack B. Jiang ,  Mary G. Johnson

    发明人： Jack B. Jiang ,  Mary G. Johnson

    IPC分类号： C07D493/04 ,  C07D519/00

    CPC分类号： C07D493/04

    摘要： The present invention provides novel furocoumarinsufonamide derivatives having the formula ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H or lower alkyl; m, n and p are independently 2, 3, 4, 5 or 6; A is NR.sub.4 (CH.sub.2).sub.P NR.sub.5, NR.sub.6, O or S; R.sub.2 is independently H, lower alkyl or a moiety of the formula ##STR2## useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

    摘要翻译： 本发明提供具有下式的新型呋喃香豆素磺酰胺衍生物：其中R 1，R 3，R 4，R 5和R 6独立地为H或低级烷基; m，n和p分别为2,3,4,5或6; A是NR4（CH2）PNR5，NR6，O或S; R2独立地是H，低级烷基或可用于抑制蛋白激酶C的式“IMAGE”的部分，并且治疗与抑制蛋白激酶C，特别是癌症肿瘤，炎性疾病，再灌注损伤和心脏功能障碍有关或受其抑制的条件。 与再灌注损伤相关。

    Bis-(hydroxyalkylamino)-anthraquinone inhibitors of protein kinase C
    3.
    发明授权
    Bis-(hydroxyalkylamino)-anthraquinone inhibitors of protein kinase C 失效
    蛋白激酶C的双 - （羟烷基氨基） - 蒽醌抑制剂

    公开(公告)号：US5204370A

    公开(公告)日：1993-04-20

    申请号：US609252

    申请日：1990-11-05

    申请人： Jack B. Jiang ,  Mary G. Johnson

    发明人： Jack B. Jiang ,  Mary G. Johnson

    IPC分类号： C07C225/34 ,  C07C225/36 ,  C07D303/36

    CPC分类号： C07C225/36 ,  C07C225/34 ,  C07D303/36

    摘要： The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl;n and m are independently 1, 2, or 3;A is Halogen, OH, alkoxy, OCO(NR.sub.3 R.sub.4), S--C(NH.sub.2).dbd.NR.sub.5, or when m=1, comprises an oxirane ring with the adjacent oxygen atom;R.sub.3, R.sub.4, and R.sub.5 are independently H, alkyl, or aryl;X is H, OH, NR.sub.6 R.sub.7, Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR.sub.8, or CONR.sub.9 R.sub.10 ; andR.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are independently H, lower alkyl, or aryluseful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

    摘要翻译： 本发明提供具有下式的新的取代的蒽醌：其中R1和R2独立地为H，C1-C10烷基，芳基，芳基烷基，烷基芳基; n和m独立地为1,2或3; A是卤素，OH，烷氧基，OCO（NR 3 R 4），S-C（NH 2）= NR 5，或当m = 1时，包含具有相邻氧原子的环氧乙烷环; R3，R4和R5独立地是H，烷基或芳基; X是H，OH，NR 6 R 7，Cl，Br，I，F，烷基，芳基，烷氧基，芳氧基，COOR 8或CONR 9 R 10; R 6，R 7，R 8，R 9和R 10独立地为可用于抑制蛋白激酶C的H，低级烷基或芳基，并且治疗与抑制蛋白激酶C特别是癌症肿瘤，炎性疾病，再灌注损伤有关或受其影响的条件 ，以及与再灌注损伤相关的心脏功能障碍。

    Bis-(hydroxylakylamino)-anthraquinone inhibitors of protein kinase C
    4.
    发明授权
    Bis-(hydroxylakylamino)-anthraquinone inhibitors of protein kinase C 失效
    蛋白激酶C的双 - （羟基烷基氨基） - 蒽醌抑制剂

    公开(公告)号：US5344841A

    公开(公告)日：1994-09-06

    申请号：US859514

    申请日：1992-06-08

    申请人： Jack B. Jiang ,  Mary G. Johnson

    发明人： Jack B. Jiang ,  Mary G. Johnson

    IPC分类号： A61K31/135 ,  A61K31/155 ,  A61K31/165 ,  A61K31/235 ,  A61K31/27 ,  A61K31/335 ,  A61K31/336 ,  A61P35/00 ,  A61P43/00 ,  C07C225/34 ,  C07C225/36 ,  C07C229/74 ,  C07C271/10 ,  C07C271/12 ,  C07C271/42 ,  C07C335/32 ,  C07D303/36 ,  A01N47/10 ,  A01N43/16

    CPC分类号： C07D303/36 ,  C07C225/34 ,  C07C225/36 ,  C07C229/74 ,  C07C271/12 ,  C07C335/32 ,  C07C2103/24

    摘要： ##STR1## The present invention provides novel substituted anthraquinones having formula (α), wherein R
    1 and R
    2 are independently H, C
    1 -C
    10 alkyl, aryl, arylalkyl, alkylaryl, or R
    1 and R
    2 taken together with the adjacent nitrogen atom N form a substituted or unsubstituted cyclic ring which may contain additional heteroatoms; n and m are independently 1, 2, or 3; A is halogen, OH, alkoxy, OCO(NR
    3 R
    4 ), S--C(NH
    2 )=NR
    5 , or when m=1, comprises an oxirane ring with the adjacent oxygen atom; R
    3 , R
    4 , and R
    5 are independently H, alkyl, or aryl; X is H, OH, NR
    6 R
    7 , Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR
    8 , or CONR
    9 R
    10 ; and R
    6 , R
    7 , R
    8 , R
    9 , and R
    10 are independently H, lower alkyl, or aryl useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

    摘要翻译： PCT No.PCT / US91 / 08026 Sec。 371日期：1992年6月8日 102（e）日期1992年6月8日PCT 1991年10月30日PCT PCT。 第WO92 / 07557号公报 （α）本发明提供具有式（α）的新的取代的蒽醌，其中R 1和R 2独立地为H，C 1 -C 10烷基，芳基，芳烷基，烷基芳基或R 1和R 2一起 与相邻的氮原子N形成可以含有其它杂原子的取代或未取代的环; n和m独立地为1,2或3; A是卤素，OH，烷氧基，OCO（NR 3 R 4），S-C（NH 2）= NR 5，或当m = 1时，包含具有相邻氧原子的环氧乙烷环; R3，R4和R5独立地是H，烷基或芳基; X是H，OH，NR 6 R 7，Cl，Br，I，F，烷基，芳基，烷氧基，芳氧基，COOR 8或CONR 9 R 10; R 6，R 7，R 8，R 9和R 10独立地为可用于抑制蛋白激酶C的H，低级烷基或芳基，并且治疗与抑制蛋白激酶C特别是癌症肿瘤，炎性疾病，再灌注损伤有关或受其影响的条件 ，以及与再灌注损伤相关的心脏功能障碍。

    1,4-bis-(amino-hydroxyalkylamino)-anthraquinones for inhibiting protein kinase C
    5.
    发明授权
    1,4-bis-(amino-hydroxyalkylamino)-anthraquinones for inhibiting protein kinase C 失效
    用于抑制蛋白激酶C的1,4-BIS-（氨基 - 羟基甲酰氨基） - 亚硝基

    公开(公告)号：US5141957A

    公开(公告)日：1992-08-25

    申请号：US609416

    申请日：1990-11-05

    申请人： Jack B. Jiang ,  Mary G. Johnson

    发明人： Jack B. Jiang ,  Mary G. Johnson

    IPC分类号： A61K31/135 ,  A61K31/165 ,  A61K31/19 ,  A61K31/24 ,  A61P7/02 ,  A61P9/00 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C20060101 ,  C07C225/34 ,  C07C225/36 ,  C07C229/74 ,  C07C237/06 ,  C12N9/99

    CPC分类号： C07C225/36 ,  C07C225/34

    摘要： The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, alkyl, aryl, or arylalkyl;m and n are independently 1, 2, or 3;X is H, OH, NR.sub.3 R.sub.4, Cl, Br, I, F, alkyl, aryl alkoxy, aroxy, COOR.sub.5, or CONR.sub.6 R.sub.7 ;R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 are independently H, lower alkyl or aryluseful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.

    摘要翻译： 本发明提供具有下式的新型取代的蒽醌：其中R 1和R 2独立地为H，烷基，芳基或芳基烷基; m和n分别为1,2或3; X是H，OH，NR 3 R 4，Cl，Br，I，F，烷基，芳基烷氧基，芳氧基，COOR 5或CONR 6 R 7; R 3，R 4，R 5，R 6和R 7独立地是H，可用于抑制蛋白激酶C的低级烷基或芳基，并且治疗与抑制蛋白激酶C特别是癌症肿瘤，炎性疾病，再灌注损伤相关或受其影响的病症 与再灌注损伤相关的心脏功能障碍。

    Substituted aurone derivatives
    6.
    发明授权
    Substituted aurone derivatives 失效
    取代的鸢尾衍生物

    公开(公告)号：US06307070B1

    公开(公告)日：2001-10-23

    申请号：US09122257

    申请日：1998-07-24

    申请人： Wai-Lam Alex Chu ,  Flemming R. Jensen ,  Thomas B. Jensen ,  James B. McAlpine ,  Birgitte Søkilde ,  Alexandra M. SantAna-Sørensen ,  Sunil Ratnayake ,  Jack B. Jiang ,  Catharine Noble ,  Angela M. Stafford

    发明人： Wai-Lam Alex Chu ,  Flemming R. Jensen ,  Thomas B. Jensen ,  James B. McAlpine ,  Birgitte Søkilde ,  Alexandra M. SantAna-Sørensen ,  Sunil Ratnayake ,  Jack B. Jiang ,  Catharine Noble ,  Angela M. Stafford

    IPC分类号： C07D30783

    CPC分类号： C07D307/82 ,  A61K31/343 ,  C07D307/83

    摘要： A method for treating a fungal infection is disclosed. The method includes administering to a patient a pharmaceutical composition containing a compound of formula (IA): where each R is independently H, OH, Br, Cl, I, amino, thiol, nitro, C1-4 alkoxy, C1-4 alkenyloxy, C2-6 alkoxyalkyleneoxy, C1-4 alkylthio, C3-18 alkyl, or C3-18 alkenyl; or two adjacent R's, taken together, are a C2-18 bivalent moiety containing at least one oxgen atom, substituted or disubstituted with A or B or both, A being H, OH, Br, Cl, I, amino, or thiol, and B being H, C1-10 alkyl, C2-18 alkenyl, or C6-18 aryl; provided at least two Rs are not H; X is C4-10 alkyl, C4-20 alkenyl, or a C4-20 single, C6-20 bridged, or C6-20 fused ring moiety containing cycloalkyl, cycloalkenyl, aryl, heterocycle, or heteroaryl, where X is substituted with H, OH, Cl, Br, I, amino, cyano, nitro, alkyl, alkoxy, alkenyl, or alkenyloxy; provided that if X is a heteroaryl or heterocyclic moiety where two Rs are each OH and meta to each other, then the remaining R is H and ortho to each of the two hydroxyls, and Y and Z are each O and a ring atom of X is linked directly to the sp2 carbon atom adjacent to X, then substituted with H, OH, Cl, Br, I, amino, cyano, alkyl, alkoxy, alkenyl, or alkenyloxy; and each of Y and Z is independently selected from O, S, and NH; or a pharmaceutically acceptable salt or ester thereof.

    摘要翻译： 公开了一种治疗真菌感染的方法。 该方法包括向患者施用含有式（IA）化合物的药物组合物：其中每个R独立地为H，OH，Br，Cl，I，氨基，硫醇，硝基，C 1-4烷氧基，C 1-4链烯氧基， C 2-6烷氧基亚烷基氧基，C 1-4烷硫基，C 3-8烷基或C 3-8烯基; 或两个相邻的R一起是含有至少一个被A或B或两者取代或二取代的氧原子的C2-18二价部分，A是H，OH，Br，Cl，I，氨基或硫醇，以及 B是H，C 1-10烷基，C 2-8烯基或C 6-18芳基; 提供至少两个R不是H; X是C 4-10烷基，C 4-20链烯基，或含有环烷基，环烯基，芳基，杂环或碳原子的C 4-20单-C6-20桥环或C6-20稠环部分 杂芳基，其中X被H，OH，Cl，Br，I，氨基，氰基，硝基，烷基，烷氧基，烯基或烯氧基取代; 条件是如果X是杂芳基或杂环部分，其中两个R 5各自为OH并且彼此相互间隔，则剩余的R是H和两个羟基中的每一个的邻位，Y和Z各自为O，X为环原子 直接与X相邻的sp2碳原子连接，然后用H，OH，Cl，Br，I，氨基，氰基，烷基，烷氧基，烯基或烯氧基取代; Y和Z各自独立地选自O，S和NH; 或其药学上可接受的盐或酯。

    Alicyclic imidazoles as H3 agents
    8.
    发明授权
    Alicyclic imidazoles as H3 agents 失效
    脂环族咪唑作为H3剂

    公开(公告)号：US06794405B2

    公开(公告)日：2004-09-21

    申请号：US10344787

    申请日：2003-08-04

    申请人： Yajing Rong ,  Jack B. Jiang ,  Syed M. Ali

    发明人： Yajing Rong ,  Jack B. Jiang ,  Syed M. Ali

    IPC分类号： A61K314164

    CPC分类号： C07D233/64

    摘要： Alicyclic imidazole compounds; pharmaceutically active compositions containing such compounds; and the use of such compounds in formulations for the control or prevention of disease states in which histamine H3 receptors are involved, such as allergy, inflammation, hypotension, glaucoma, sleeping disorders, states of hyper- and hypo-motility of the gastro-intestinal tract, cardiovascular disease, hypo- and hyper-activity of the central nervous system, Alzheimer's, schizophrenia, obesity and migraines are disclosed.

    摘要翻译： 脂环咪唑化合物; 含有这些化合物的药物活性组合物; 以及这些化合物在制剂中的用途，用于控制或预防其中涉及组胺H3受体的疾病状态，例如过敏，炎症，低血压，青光眼，睡眠障碍，胃肠超和运动不足的状态 公开了中枢神经系统，阿尔茨海默病，精神分裂症，肥胖症和偏头痛的低血压，高血压，心脑血管疾病，低血压和高活性。